LP46

LP46 : Inhibitor of IKBKB

Structure

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Information

IKBKB

Inhibitor

up to 5 µM

In Vitro Validations

Uniprot ID: O14920

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 7.5 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Inhibitor of nuclear factor kappa-B kinase subunit ...

DOI Reference: 10.1021/acs.jmedchem.5c01938

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Screening against a panel of 97 kinases across the kinome, LP46 @ 100 nM displayed the highest binding affinity for IKKβ, with a selectivity for IKKβ over its homologue IKKα (IC50 = 46.9 nM) of approximately 6.3-fold. Furthermore, the S-score (35) of LP46 was 0.05 and the S-score (10) was 0.02.

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